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| 5mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
Calcipotriol (MC-903; Daivonex; Dovonex; PRI-2201; Psorcutan; Sorilux) is a synthetic calcitriol/Vitamin D3 (VD3) analog and an agonist of the VD3 receptor. It is used in the treatment of psoriasis and marketed under the trade name Dovonex. It has comparable affinity with calcitriol (Vit. D) for the Vitamin D receptor (VDR), while being less than 1% as active as the calcitriol in regulating calcium metabolism. Chronic plaque psoriasis is the chief medical use of calcipotriol. It has also been used successfully in the treatment of alopecia areata.
| ln Vitro |
In the absence of IL-17A or IL-22 stimulation, calcipotriol either had no effect (2–20 nM) or only slightly increased (0.2 nM) the expression of IL-8 mRNA in NHEK cells. Our earlier research was validated by the addition of IL-17A and IL-22, which greatly raised the mRNA expression of IL-8. In a dose-dependent manner, 2, 20, and 40 nM calcipotriol can suppress this increased IL-8 mRNA expression [1]. The expression of NK cytotoxic receptors, or KIRs, is modulated when medicines are administered to natural killer (NK) cells. For four hours, calcipotriol, FTY720, or 100, 10, or 1 ng/mL of 1,25(OH)2D3 were applied as a pretreatment to human NK cells. Following a 4-hour incubation period, the expression of NKp30 on the surface of NK cells was considerably elevated by all three doses of 1,25(OH)2D3, calcipotriol, and FTY720 [2].
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| ln Vivo |
The diclofenac plus DFMO plus calcipotriol group resulted in 1 out of every 32 animals dying, whereas all other animals in this group survived. Every group had a similar survival rate. Diclofenac plus calcipotriol (p=0.018) and diclofenac plus DFMO plus calcipotriol (p=0.002) therapy groups showed considerably less weight gain when compared to the placebo (linear regression model) [3].
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| References |
[1]. Sakabe JI, et al. Calcipotriol Increases hCAP18 mRNA Expression but Inhibits Extracellular LL37 Peptide Production in IL-17/IL-22-stimulated Normal Human Epidermal Keratinocytes. Acta Derm Venereol. 2014 Sep;94(5):512-6.
[2]. Al-Jaderi Z, et al. Effects of vitamin D3, calcipotriol and FTY720 on the expression of surface molecules and cytolytic activities of human natural killer cells and dendritic cells. Toxins (Basel). 2013 Oct 28;5(11):1932-47. [3]. Pommergaard HC, et al. Combination chemoprevention with diclofenac, calcipotriol and difluoromethylornithine inhibits development of non-melanoma skin cancer in mice. Anticancer Res. 2013 Aug;33(8):3033-9. [4]. Reinhard Bredehorst, et al. Induction of Antigen-Specific Tolerance by Peripheral Phagocytosis. US 20150283231 A1. [5]. Kaur A, et al. Nanoemulsion loaded gel for topical co-delivery of clobitasol propionate and calcipotriol in psoriasis. Nanomedicine. 2017 May;13(4):1473-1482 |
| Molecular Formula |
C27H40O3
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|---|---|
| Molecular Weight |
412.61
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| CAS # |
112965-21-6
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| Related CAS # |
Calcipotriol monohydrate;147657-22-5;Impurity F of Calcipotriol;112875-61-3
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| SMILES |
C[C@H](/C=C/[C@H](C1CC1)O)[C@H]([C@]2(CCC/3)C)CC[C@@]2([H])C3=C\C=C4C[C@H](O)C[C@@H](O)C\4=C
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| InChi Key |
LWQQLNNNIPYSNX-JQWURIRRSA-N
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| InChi Code |
InChI=1S/C27H40O3/c1-17(6-13-25(29)20-8-9-20)23-11-12-24-19(5-4-14-27(23,24)3)7-10-21-15-22(28)16-26(30)18(21)2/h6-7,10,13,17,20,22-26,28-30H,2,4-5,8-9,11-12,14-16H2,1,3H3/b13-6+,19-7+,21-10-/t17-,22+,23-,24+,25-,26-,27-/m1/s1
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| Chemical Name |
(5Z,7E,22E,24S)-24-Cyclopropyl-9,10-secochola-5,7,10(19),22-tetraene-1alpha,3beta,24-triol
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| Synonyms |
Calcipotriene calcipotriol MC-903PRI 2201MC903PRI-2201Calcitrene CCRIS
7700 Daivonex Dovonex MC 903 Psorcutan Sorilux.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~242.37 mM)
Ethanol : ~50 mg/mL (~121.18 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4236 mL | 12.1180 mL | 24.2360 mL | |
| 5 mM | 0.4847 mL | 2.4236 mL | 4.8472 mL | |
| 10 mM | 0.2424 mL | 1.2118 mL | 2.4236 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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